CN103958480B - 咪唑啉类衍生物、其制备方法及其在医药上的应用 - Google Patents
咪唑啉类衍生物、其制备方法及其在医药上的应用 Download PDFInfo
- Publication number
- CN103958480B CN103958480B CN201380004069.5A CN201380004069A CN103958480B CN 103958480 B CN103958480 B CN 103958480B CN 201380004069 A CN201380004069 A CN 201380004069A CN 103958480 B CN103958480 B CN 103958480B
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- China
- Prior art keywords
- dimethyl
- trifluoromethyl
- thioimidazolin
- benzonitrile
- general formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 0 *C(C(N(C1=*)c2ccc(*)c(*)c2)=*)(N1c(cc1*)ccc1O)I Chemical compound *C(C(N(C1=*)c2ccc(*)c(*)c2)=*)(N1c(cc1*)ccc1O)I 0.000 description 11
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- KWUBVEVDMHJJSA-UHFFFAOYSA-N C(C1)[N]11CC(CCC2)C2CCC1 Chemical compound C(C1)[N]11CC(CCC2)C2CCC1 KWUBVEVDMHJJSA-UHFFFAOYSA-N 0.000 description 1
- MZFQJBMXUXJUHF-UHFFFAOYSA-N C1C2C1CCNC2 Chemical compound C1C2C1CCNC2 MZFQJBMXUXJUHF-UHFFFAOYSA-N 0.000 description 1
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- JOAUMQMXRCJIOL-UHFFFAOYSA-N CC(C)(C(N(C1=S)c(cc2)cc(C(F)(F)F)c2C#N)=O)N1c(cn1)ccc1OCCO Chemical compound CC(C)(C(N(C1=S)c(cc2)cc(C(F)(F)F)c2C#N)=O)N1c(cn1)ccc1OCCO JOAUMQMXRCJIOL-UHFFFAOYSA-N 0.000 description 1
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- CCRYQZVWJHGRDN-KKFHFHRHSA-N CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cc1)cc(F)c1OC(COC1)[C@H]1O Chemical compound CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cc1)cc(F)c1OC(COC1)[C@H]1O CCRYQZVWJHGRDN-KKFHFHRHSA-N 0.000 description 1
- REAYPDANMJMTHI-UHFFFAOYSA-N CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cc1)ccc1OCCO Chemical compound CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cc1)ccc1OCCO REAYPDANMJMTHI-UHFFFAOYSA-N 0.000 description 1
- IJVGPJWSXBHYLC-UHFFFAOYSA-N CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cn1)ccc1O Chemical compound CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cn1)ccc1O IJVGPJWSXBHYLC-UHFFFAOYSA-N 0.000 description 1
- HSURGBKROROPOM-MRXNPFEDSA-N CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cn1)ccc1O[C@H]1COCC1 Chemical compound CC(C)(C(N(C1=S)c(cc2C(F)(F)F)ccc2C#N)=O)N1c(cn1)ccc1O[C@H]1COCC1 HSURGBKROROPOM-MRXNPFEDSA-N 0.000 description 1
- CNNNWVYABYOKQS-LROBGIAVSA-N CC(C)(C(N(C1=S)c(cc2C)ccc2C#N)=O)N1c(cc1)cc(F)c1OC(COC1)[C@H]1O Chemical compound CC(C)(C(N(C1=S)c(cc2C)ccc2C#N)=O)N1c(cc1)cc(F)c1OC(COC1)[C@H]1O CNNNWVYABYOKQS-LROBGIAVSA-N 0.000 description 1
- WJKQBPVBUSEJDV-UHFFFAOYSA-N CC(C)(C(N(C1=S)c(cc2C)ccc2C#N)=O)N1c(cc1)ccc1OCCO Chemical compound CC(C)(C(N(C1=S)c(cc2C)ccc2C#N)=O)N1c(cc1)ccc1OCCO WJKQBPVBUSEJDV-UHFFFAOYSA-N 0.000 description 1
- ASHCMGMNYBEOJJ-UHFFFAOYSA-N CC(C)(C)[Si](C)(C)OCCOc(nc1)ccc1N(C(C)(C)C(N1c(cc2C(F)(F)F)ccc2C#N)=O)C1=S Chemical compound CC(C)(C)[Si](C)(C)OCCOc(nc1)ccc1N(C(C)(C)C(N1c(cc2C(F)(F)F)ccc2C#N)=O)C1=S ASHCMGMNYBEOJJ-UHFFFAOYSA-N 0.000 description 1
- ISTPGKKWPYNSDT-UHFFFAOYSA-O Cc(cc1)ccc1S([OH2+])(/[O]=C1\COCC1)=O Chemical compound Cc(cc1)ccc1S([OH2+])(/[O]=C1\COCC1)=O ISTPGKKWPYNSDT-UHFFFAOYSA-O 0.000 description 1
- BHNHHSOHWZKFOX-UHFFFAOYSA-N Cc1cc2ccccc2[nH]1 Chemical compound Cc1cc2ccccc2[nH]1 BHNHHSOHWZKFOX-UHFFFAOYSA-N 0.000 description 1
- LQJJUUPOFDPWOA-UHFFFAOYSA-N NC(C1)CN2C1COCC2 Chemical compound NC(C1)CN2C1COCC2 LQJJUUPOFDPWOA-UHFFFAOYSA-N 0.000 description 1
- HAAZJWVQKLGNDT-UHFFFAOYSA-N O=C1N(CCC2)C2CNC1 Chemical compound O=C1N(CCC2)C2CNC1 HAAZJWVQKLGNDT-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
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- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A61K31/4164—1,3-Diazoles
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201380004069.5A CN103958480B (zh) | 2012-09-04 | 2013-08-26 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210323870.3 | 2012-09-04 | ||
| CN2012103238703 | 2012-09-04 | ||
| CN201210323870 | 2012-09-04 | ||
| PCT/CN2013/082273 WO2014036897A1 (zh) | 2012-09-04 | 2013-08-26 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
| CN201380004069.5A CN103958480B (zh) | 2012-09-04 | 2013-08-26 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103958480A CN103958480A (zh) | 2014-07-30 |
| CN103958480B true CN103958480B (zh) | 2016-04-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380004069.5A Active CN103958480B (zh) | 2012-09-04 | 2013-08-26 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9586947B2 (https=) |
| EP (1) | EP2894151B1 (https=) |
| JP (1) | JP6262733B2 (https=) |
| KR (1) | KR102189940B1 (https=) |
| CN (1) | CN103958480B (https=) |
| AU (1) | AU2013312587B2 (https=) |
| BR (1) | BR112015004637B1 (https=) |
| CA (1) | CA2883545C (https=) |
| CY (1) | CY1123649T1 (https=) |
| DK (1) | DK2894151T3 (https=) |
| ES (1) | ES2835248T3 (https=) |
| HR (1) | HRP20202050T1 (https=) |
| HU (1) | HUE052904T2 (https=) |
| LT (1) | LT2894151T (https=) |
| MX (1) | MX368844B (https=) |
| PT (1) | PT2894151T (https=) |
| RS (1) | RS61242B1 (https=) |
| RU (1) | RU2639145C2 (https=) |
| SI (1) | SI2894151T1 (https=) |
| SM (1) | SMT202000672T1 (https=) |
| TW (1) | TWI617546B (https=) |
| WO (1) | WO2014036897A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014036897A1 (zh) * | 2012-09-04 | 2014-03-13 | 上海恒瑞医药有限公司 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
| JP6817962B2 (ja) * | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
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